TW202043225A - B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 - Google Patents

B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 Download PDF

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TW202043225A
TW202043225A TW109102401A TW109102401A TW202043225A TW 202043225 A TW202043225 A TW 202043225A TW 109102401 A TW109102401 A TW 109102401A TW 109102401 A TW109102401 A TW 109102401A TW 202043225 A TW202043225 A TW 202043225A
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compound
hpmcas
free base
weight ratio
solid dispersion
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TW109102401A
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Chinese (zh)
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張國良
昌友 周
孫熀彬
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英屬開曼群島商百濟神州有限公司
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Dispersion Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW109102401A 2019-01-25 2020-01-22 B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 TW202043225A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
WOPCT/CN2019/073254 2019-01-25
CN2019073254 2019-01-25
CN2019095227 2019-07-09
WOPCT/CN2019/095227 2019-07-09

Publications (1)

Publication Number Publication Date
TW202043225A true TW202043225A (zh) 2020-12-01

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Application Number Title Priority Date Filing Date
TW109102401A TW202043225A (zh) 2019-01-25 2020-01-22 B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途

Country Status (14)

Country Link
US (1) US20220105033A1 (pt)
EP (1) EP3914591A4 (pt)
JP (1) JP2022517675A (pt)
KR (1) KR20210120039A (pt)
CN (1) CN113330011A (pt)
AU (1) AU2020211000A1 (pt)
BR (1) BR112021014563A2 (pt)
CA (1) CA3123476A1 (pt)
IL (1) IL284636A (pt)
MX (1) MX2021008884A (pt)
SG (1) SG11202107849RA (pt)
TW (1) TW202043225A (pt)
WO (1) WO2020151756A1 (pt)
ZA (1) ZA202104032B (pt)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230036929A (ko) 2021-09-08 2023-03-15 주식회사 엘지에너지솔루션 배터리 진단 장치, 배터리 관리 시스템, 배터리 팩, 전기 차량 및 배터리 진단 방법
CN114366717B (zh) * 2022-01-11 2023-06-09 四川农业大学 一种基于egcg纳米粒的肠溶固体分散体颗粒、制备方法及其应用
WO2023240178A1 (en) * 2022-06-08 2023-12-14 Mapkure, Llc Methods of treating cancer with a b-raf inhibitor
WO2024073364A1 (en) * 2022-09-26 2024-04-04 Beigene, Ltd. Combinations of a b-raf inhibitor, and an anti-egfr antibody for the treatment of cancer

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY161576A (en) * 2008-03-17 2017-04-28 Ambit Biosciences Corp Quinazoline derivatives as raf kinase modulators and methods of use thereof
CR20170089A (es) * 2009-04-03 2017-07-17 Plexxikon Inc Composiciones del acido propano-1--sulfonico {3-[5-(4-cloro-fenil)-1h-pirrolo [2,3-b] piridina-3-carbonil] -2,4-difluoro-fenil}-amida y el uso de las mismas
SG178854A1 (en) * 2009-08-28 2012-04-27 Array Biopharma Inc Raf inhibitor compounds and methods of use thereof
RS58455B1 (sr) * 2011-02-07 2019-04-30 Plexxikon Inc Jedinjenja i postupci za modulaciju kinaze, i indikacije za njih
PT2882440T (pt) * 2012-08-07 2019-04-23 Array Biopharma Inc Combinações farmacêuticas compreendendo um inibidor de braf, um inibidor de egfr e opcionalmente um inibidor de pi3k-alfa
PE20151335A1 (es) * 2013-01-22 2015-09-18 Hoffmann La Roche Composicion farmaceutica con biodisponibilidad mejorada
EP3013798B1 (en) * 2013-06-28 2018-06-27 BeiGene, Ltd. Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors
EP3013797B1 (en) * 2013-06-28 2018-01-03 BeiGene, Ltd. Fused tricyclic amide compounds as multiple kinase inhibitors
WO2015152433A1 (en) * 2014-03-31 2015-10-08 Hanmi Pharm. Co., Ltd. Amorphous solid dispersion comprising paclitaxel, tablet comprising the same, and method for preparing the same

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Publication number Publication date
SG11202107849RA (en) 2021-08-30
ZA202104032B (en) 2022-08-31
EP3914591A4 (en) 2022-11-09
US20220105033A1 (en) 2022-04-07
CA3123476A1 (en) 2020-07-30
EP3914591A1 (en) 2021-12-01
MX2021008884A (es) 2021-08-19
KR20210120039A (ko) 2021-10-06
BR112021014563A2 (pt) 2021-10-05
WO2020151756A1 (en) 2020-07-30
AU2020211000A1 (en) 2021-08-12
IL284636A (en) 2021-08-31
JP2022517675A (ja) 2022-03-09
CN113330011A (zh) 2021-08-31

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